1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Deubiquitinase

Deubiquitinase

Deubiquitinases (DUBs) are a family of proteases whose function is to cleave ubiquitin (Ub) or ubiquitin-like proteins from proproteins or ubiquitin(s) conjugated with target substrate. DUBs are divided into two main classes according to their enzymatic cleavage mechanism: cysteine proteases and zinc metalloproteases. These include ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), ovarian tumor proteases (OTUs), Machado-Joseph disease proteases (MJDs), Jab1/Mov34/Mpr1 (JAMM) metalloproteases, and MIU-containing novel DUB family, (MINDY) proteases.

Ubiquitination is an important post-translational modification that plays a key role in many vital cellular events. In this process, ubiquitin is attached to a substrate protein by the concerted action of an enzyme cascade involving E1, E2 and E3 enzymes and it is removed by DUBs. DUBs are therefore important regulators of the Ub system and regulate a plethora of cellular processes, including protein turnover, protein sorting, and trafficking. Altered DUB activity is associated with a multitude of pathologies including cancer. DUBs represent novel candidates for target-directed drug development.

Deubiquitinase Related Products (41):

Cat. No. Product Name Effect Purity
  • HY-13453
    BAY 11-7082 Inhibitor 99.98%
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-D0843
    N-Ethylmaleimide Inhibitor ≥98.0%
    N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
  • HY-13814
    PR-619 Inhibitor 98.89%
    PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.
  • HY-117043
    GRL0617 Inhibitor 99.78%
    GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro)/deubiquitinase, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM.
  • HY-107985
    FT671 Inhibitor 99.79%
    FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
  • HY-134817
    USP7-IN-8 Inhibitor ≥98.0%
    USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.
  • HY-111408
    EOAI3402143 Inhibitor 99.52%
    EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
  • HY-13264
    Degrasyn Inhibitor ≥98.0%
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
  • HY-100900
    ML364 Inhibitor 99.94%
    ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
  • HY-13765
    6-Thioguanine Inhibitor ≥99.0%
    6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
  • HY-15667
    P005091 Inhibitor 99.94%
    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
  • HY-107986
    GNE-6776 Inhibitor 98.29%
    GNE-6776 is a selective and orally bioavailable USP7 inhibitor.
  • HY-13865
    P 22077 Inhibitor 99.97%
    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.
  • HY-112937
    GNE-6640 Inhibitor 99.96%
    GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.
  • HY-17543
    ML-323 Inhibitor 99.97%
    ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
  • HY-50737A
    DUB-IN-2 Inhibitor 98.72%
    DUB-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.
  • HY-13989
    b-AP15 Inhibitor 98.75%
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
  • HY-13817
    IU1 Inhibitor ≥98.0%
    IU1 is a special Usp14 inhibitor with an IC50 of 4-5 μM.
  • HY-117370
    USP25/28 inhibitor AZ1 Inhibitor 98.10%
    USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
  • HY-111458
    GSK2643943A Inhibitor 98.31%
    GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC50 of 160 nM for USP20/Ub-Rho.
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